Figure 10. Structures (A) and competitive ABPP inhibition profiles (B) of ABHD11 inhibitors WWL222 (SID 124343013) and ML226.

Figure 10Structures (A) and competitive ABPP inhibition profiles (B) of ABHD11 inhibitors WWL222 (SID 124343013) and ML226.

Gel-based competitive ABPP assay (B) conducted as described in AID 504892 with recombinant human ABHD11 spiked into mouse brain membrane proteome. For ML226, 75% and 100% inhibition of human ABHD11 is observed at 30 nM and 150 nM compound concentration, respectively, whereas no inhibition of human ABHD11 is observed upon treatment with 20 μM WWL222. No enzyme = mouse brain membrane proteome alone with FP-Rh labeling; Control = 0 compound (DMSO only). Fluorescent image shown in grey scale.

From: Optimization and characterization of a triazole urea inhibitor for alpha/beta hydrolase domain-containing protein 11 (ABHD11): anti-probe for LYPLA1/LYPLA2 dual inhibitor ML211

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